Chitosan films and hydrogels of chlorhexidine gluconate for oral mucosal delivery

Topical delivery of antimicrobial agents is the most widely accepted approa ch aimed at prolonging active drug concentrations in the oral cavity. As mo st antifungals do not posses inherent ability to bind to the oral mucosa, t his is best achieved through improved formulations. Chitosan, a partially d eacetylated chitin, which is a biologically safe biopolymer, prolongs the a dhesion time of oral gels and drug release from them. Chitosan also inhibit s the adhesion of Candida albicans to human buccal cells and has antifungal activity. The antifungal agent, chlorhexidine gluconate (Chx), also reduce s C. albicans adhesion to oral mucosal cells. The aim of this study was to design a formulation containing chitosan for local delivery of Chx to the o ral cavity. Gels (at 1 or 2% concentration) or him forms of chitosan were p repared containing 0.1 or 0.2% Chx and their in vitro release properties we re studied. The antifungal activity of chitosan itself as well as the vario us formulations containing Chx was also examined. Release of Chx from gels was maintained for 3 h. A prolonged release was observed with film formulat ions. No lag-time was observed in release of Chx from either gels or films. The highest antifungal activity was obtained with 2% chitosan gel containi ng 0.1% Chx. (C) 2000 Elsevier Science B.V. All rights reserved.